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公开(公告)号：EP1315736A2
公开(公告)日：2003-06-04
申请号：EP01976128.7
申请日：2001-08-21
发明人： DEVOS, Rene , DYMOCK, Brian William , HOBBS, Christopher John , JIANG, Wen-Rong , MARTIN, Joseph Armstrong , MERRETT, John Herbert , NAJERA, Isabel , SHIMMA, Nobuo , TSUKUDA, Takuo
IPC分类号： C07H19/06 , C07H19/16 , A61K31/7064 , A61K31/7076 , A61P31/14
摘要： Use of compounds of formula (I), wherein R1 is hydrogen, hydroxy, alkyl, hydroxyalkyl, alkoxy, halogen, cyano, isocyano or azido; R2 is hydrogen, hydroxy, alkoxy, chlorine, bromine or iodine; R3 is hydrogen; or R?2 and R3¿ together represent =CH¿2?; or R?2 and R3¿ represent fluorine; X is O, s or CH¿2?; a, b, c, d denoting asymmetric carbon atoms each of which is substituted with 4 different substituents; and B signifies a purine base B1 which is connected through the 9-nitrogen of formula (B1), wherein R?4¿ is hydrogen, hydroxyl, alkyl, alkoxy, alkylthio, aryloxy, arylthio, heterocyclyl, NR7R8, halogen or SH; R5 is hydrogen, hydroxy, alkyl, haloalkyl, cycloalkyl, alkoxy, alkylthio, aryl, aryloxy, arylthio, heterocyclyl, heterocyclylamino, halogen, NR?7R8, NHOR9, NHNR7R8¿ or SH; R6 is hydrogen, hydroxy, alkyl, alkoxy, alkylthio, aryloxy, arylthio, heterocyclyl, NR7R8, halogen, SH or cyano; R?7 and R8¿ are independently of each other hydrogen, alkyl, aryl, hydroxyalkyl, alkenylalkyl, alkynylalkyl, cycloalkyl or acyl; R9 is hydrogen, alkyl or aryl; or B signifies an oxidised purine base B2 which is connected through the 9-nitrogen of formula (B2), wherein R?4, R5 and R6¿ are as defined above; or B signifies a purine base B3 which is connected through the 9-nitrogen of formula (B3), wherein R?4 and R6¿ are as defined above; R10 is hydrogen, alkyl or aryl; Y is O, S or NR11; R11 is hydrogen, hydroxy, alkyl, OR9, heterocyclyl or NR?7R8; R7, R8 and R9¿ are as defined above; or B signifies a pyrimidine base B4 which is connected through the 1-nitrogen of formula (B4), wherein Z is O or S; R12 is hydrogen, hydroxy, alkyl, alkoxy, haloalkyl, alkylthio, aryl, aryloxy, arylthio, heterocyclyl, heterocyclylamino, halogen, NR?7R8, NHOR9, NHNR7R8¿ or SH; R13 is hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl, haloalkyl, cycloalkyl or halogen; R?7, R8 and R9¿ are as defined above; or B signifies a pyrimidine base B5 which is connected through the 1-nitrogen of formula (B5), wherein Y, Z, R10 are as defined above for the treatment of diseases mediated by the Hepatitis C Virus (HIV) or for the preparation of a medicament for such treatment. The invention is concerned with novel and known purine and pyrimidine nucleoside derivatives, their use as inhibitors of subgenomic Hepatitis C Virus (HCV) RNA replication and pharmaceutical compositions of such compounds.
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公开(公告)号：EP1301481A1
公开(公告)日：2003-04-16
申请号：EP01938137.5
申请日：2001-04-30
IPC分类号： C07D207/36 , C07D401/06 , A61K31/44 , A61K31/40 , A61K31/18
CPC分类号： C07D401/06 , C07D207/36 , C07D401/14 , C07D409/06 , C07D417/06
摘要： The invention is concerned with novel pyrrole derivatives, a prcess for their manufacture, pharmaceutical compositions and the use of such compounds in medecine. In particular, the compounds of formula (I) are inhibitors of the human immunodeficiency virus reverse transcriptase enzyme which is involved in viral replication. Consequently the compounds of this invention may be advantageously used as therapeutic agents for HIV mediated process. The invention describes novel compounds of formula (I) wherein R1 is alkyl, cycloalkyl, aryl or heterocyclyl; R2 is alkyl, cycloalkyl, aryl or heterocyclyl; R3 is hydrogen, alkyl, cycloalkyl, aryl or heterocyclyl; R4 is hydrogen, alkyl, carboxyl, C(=O)R, CONR'R'', cyano or alkenyl, wherein R is hydrogen, alkyl, alkoxy, trifluoromethyl, methyl-oxy-carbonyl or ethyl-oxy-carbonyl, and wherein R' and R'', are independantly of each other, hydrogen, alkyl or aryl; R5 is alkyl, aryl or a group -Z-C(=O)R''', wherein Z is a single bond or -CH=CH-, and wherein R''' is hydrogen or alkyl; X represents S, S(O), S(O)¿2?, O, N(alkyl) or X-R?2¿ together CH¿2?-aryl or CH2-heterocyclyl; and with the proviso that only one of R?3 and R4¿ is hydrogen and alkyl in R3 is not CF¿3?; and hydrolyzable esters or ethers thereof or a pharmaceutically acceptable salt thereof.
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